AR049536A1 - Compuestos heterociclicos condensados con actividad inhibitoria de la proteina tirosina cinasa; una composicion farmaceutica que los contiene como principio activo y su utilizacion en el tratamiento del cancer. - Google Patents
Compuestos heterociclicos condensados con actividad inhibitoria de la proteina tirosina cinasa; una composicion farmaceutica que los contiene como principio activo y su utilizacion en el tratamiento del cancer.Info
- Publication number
- AR049536A1 AR049536A1 ARP050102668A ARP050102668A AR049536A1 AR 049536 A1 AR049536 A1 AR 049536A1 AR P050102668 A ARP050102668 A AR P050102668A AR P050102668 A ARP050102668 A AR P050102668A AR 049536 A1 AR049536 A1 AR 049536A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- alkyl
- heteroaryl
- aryl
- heterocycloalkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 206010028980 Neoplasm Diseases 0.000 title abstract 2
- 201000011510 cancer Diseases 0.000 title abstract 2
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 title 1
- 230000002401 inhibitory effect Effects 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 102000004169 proteins and genes Human genes 0.000 title 1
- 108090000623 proteins and genes Proteins 0.000 title 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 title 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 18
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 16
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 10
- 125000003118 aryl group Chemical group 0.000 abstract 9
- 125000003107 substituted aryl group Chemical group 0.000 abstract 9
- 125000000217 alkyl group Chemical group 0.000 abstract 8
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 8
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 7
- 125000000623 heterocyclic group Chemical group 0.000 abstract 7
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000005017 substituted alkenyl group Chemical group 0.000 abstract 2
- 125000004426 substituted alkynyl group Chemical group 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 1
- 125000000278 alkyl amino alkyl group Chemical group 0.000 abstract 1
- -1 alkylaminoalkynyl Chemical group 0.000 abstract 1
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 239000003909 protein kinase inhibitor Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000565 sulfonamide group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/28—Oxygen atom
- C07D473/30—Oxygen atom attached in position 6, e.g. hypoxanthine
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Transplantation (AREA)
- Virology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Ophthalmology & Optometry (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Vascular Medicine (AREA)
Abstract
Los compuestos son utiles como inhibidores de la proteína cinasa y por lo tanto son utiles para el tratamiento del cáncer y de otras enfermedades mediada por la proteína cinasa. Reivindicacion 1: Un compuesto que tiene la formula (1) o (2) que incluye sales farmacéuticamente aceptables del mismo caracterizado porque: R1 es H, alquilo, alquilo substituido, cicloalquilo, cicloalquilo substituido, arilalquilo, arilalquilo substituido, arilo, arilo substituido, alquenilo, alquenilo substituido, alquinilo, alquinilo substituido, heteroarilo, heteroarilo substituido, heterociclo, heterociclo substituido, heteroarilalquilo, heteroarilalquilo substituido, heterocicloalquilo o heterocicloalquilo substituido; cada R2 es independientemente, H, halogeno, ciano, NO2, OR5, NR6R7, alquilo, alquilo substituido, cicloalquilo, cicloalquilo substituido, arilo, arilo substituido, heteroarilo, heteroarilo substituido, heterociclo, heterociclo substituido, arilalquilo, arilalquilo substituido, heterocicloalquilo, o heterocicloalquilo substituido; B es O, NR8, S, SO, SO2, CR9R10; V es NR11 o -(CR47R48)p-; W o X son independientemente C o N; Y es O, S, o NR12; Z es -CR13R14-, -(CR13R14)mNR15-; l es 0 hasta 4; m es 0 hasta 2; n es 0 hasta 4; p es 0 hasta 4, con la condicion de que si p es 0, R1 no es fenilo; A es un resto de formula (3) a (11); Q es CR19; D es CR20 o N; G es S, O, o NR21, con la condicion de que si A es un resto de formula (4) o de formula (5) y G es S, R4 no es un grupo fenilo substituido; R3, R5, R6, R7, R8, R11 y R15 son cada uno independientemente H, alquilo, alquilo substituido, cicloalquilo, cicloalquilo substituido, arilo, arilo substituido, heteroarilo, heteroarilo substituido, heterocicloalquilo, o heterocicloalquilo substituido; R4 es arilo, arilo substituido, heteroarilo, heteroarilo substituido, heterocicloalquilo, o heterocicloalquilo substituido; R9 y R10 son independientemente H, halogeno, alquilo, alquilo substituido, cicloalquilo, cicloalquilo substituido, arilo, arilo substituido, heteroarilo, heteroarilo substituido, heterocicloalquilo, o heterocicloalquilo substituido; R12 es H, alquilo, alquilo substituido, CN, NO2 o SO2NH2; R13, R14, R15, R47 y R48 son independientemente H, halogeno, alquilo, alquilo substituido, cicloalquilo, cicloalquilo substituido, arilo, arilo substituido, heteroarilo, heteroarilo substituido, heterociclo, heterociclo substituido o tomados juntos para formar un anillo heterocíclico o carbocíclico desde 3 hasta 8 átomos; R16, R17, R18, R20, R22, R23, R60, R61, R62, R63, R64, R65, R66, R67, R68, R69, R70, R75, R76, R78, y R79, son independientemente H, halogeno, NO2, ciano, OR26, NR27R28, CO2R29, C(O)NR30R31, SO2R32, SO2NR33R34, NR35SO2R36, NR37C(O)R38, NR39CO2R40, -CO(CH2)lR41; -CONH(CH2)lR42, alquilaminoalquilo, alquilaminoalquinilo, alquilo C1-6, alquilo C1-6 substituido, cicloalquilo C3-7, cicloalquilo C3-7 substituido, alquenilo, alquenilo substituido, alquinilo, alquinilo substituido, hidroxialquilo, arilo, arilo substituido, heteroarilo, heteroarilo substituido, arilalquilo, arilalquilo substituido, heterocicloalquilo, o heterocicloalquilo substituido; R19 es H o ciano; R21 y R24 son independientemente H, alquilo C1-6, o alquilo C1-6 substituido; R25, R74 y R77 son independientemente H, alquilo, alquilo substituido, cicloalquilo, cicloalquilo substituido, arilo, arilo substituido, arilalquilo, arilalquilo substituido, heteroarilo, heteroarilo substituido, heterocicloalquilo, o heterocicloalquilo substituido; R26, R27, R28, R29, R30, R31, R32, R33, R34, R35, R36, R37, R38, R39, R40, R41, y R42 son independientemente H, alquilo, alquilo substituido, cicloalquilo, cicloalquilo substituido, arilo, arilo substituido, arilalquilo, arilalquilo substituido, heteroarilo, heteroarilo substituido, heterocicloalquilo, o heterocicloalquilo substituido.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US58345904P | 2004-06-28 | 2004-06-28 | |
| US61256304P | 2004-09-23 | 2004-09-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR049536A1 true AR049536A1 (es) | 2006-08-09 |
Family
ID=35457856
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050102668A AR049536A1 (es) | 2004-06-28 | 2005-06-28 | Compuestos heterociclicos condensados con actividad inhibitoria de la proteina tirosina cinasa; una composicion farmaceutica que los contiene como principio activo y su utilizacion en el tratamiento del cancer. |
| ARP050102669A AR050254A1 (es) | 2004-06-28 | 2005-06-28 | Intermediarios y procesos para preparar dichos intermediarios utiles en la fabricacion de pirrolotriazinas |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050102669A AR050254A1 (es) | 2004-06-28 | 2005-06-28 | Intermediarios y procesos para preparar dichos intermediarios utiles en la fabricacion de pirrolotriazinas |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US7173031B2 (es) |
| EP (3) | EP1761268A4 (es) |
| JP (3) | JP2008504368A (es) |
| KR (3) | KR20070026621A (es) |
| AR (2) | AR049536A1 (es) |
| AU (2) | AU2005260056B2 (es) |
| BR (1) | BRPI0512722A (es) |
| CA (1) | CA2571680A1 (es) |
| IL (1) | IL180325A0 (es) |
| MX (2) | MXPA06015032A (es) |
| NO (3) | NO20070453L (es) |
| PE (2) | PE20060374A1 (es) |
| TW (2) | TW200604184A (es) |
| WO (3) | WO2006004884A2 (es) |
Families Citing this family (113)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7030112B2 (en) * | 2003-03-25 | 2006-04-18 | Bristol-Myers Squibb Company | Pyrrolopyridazine compounds and methods of use thereof for the treatment of proliferative disorders |
| US9169406B2 (en) * | 2003-08-25 | 2015-10-27 | Dow Global Technologies Llc | Coating compositions |
| PT2213661E (pt) | 2003-09-26 | 2011-12-15 | Exelixis Inc | Moduladores de c-met e métodos de uso |
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-
2005
- 2005-06-24 US US11/167,049 patent/US7173031B2/en not_active Expired - Lifetime
- 2005-06-24 US US11/167,043 patent/US20050288290A1/en not_active Abandoned
- 2005-06-27 TW TW094121497A patent/TW200604184A/zh unknown
- 2005-06-27 TW TW094121488A patent/TW200607505A/zh unknown
- 2005-06-28 WO PCT/US2005/023198 patent/WO2006004884A2/en not_active Ceased
- 2005-06-28 EP EP05791275A patent/EP1761268A4/en not_active Withdrawn
- 2005-06-28 PE PE2005000752A patent/PE20060374A1/es not_active Application Discontinuation
- 2005-06-28 CA CA002571680A patent/CA2571680A1/en not_active Abandoned
- 2005-06-28 EP EP05790229A patent/EP1771177A4/en not_active Withdrawn
- 2005-06-28 KR KR1020067026897A patent/KR20070026621A/ko not_active Withdrawn
- 2005-06-28 AR ARP050102668A patent/AR049536A1/es not_active Application Discontinuation
- 2005-06-28 WO PCT/US2005/023099 patent/WO2006004833A2/en not_active Ceased
- 2005-06-28 AR ARP050102669A patent/AR050254A1/es not_active Application Discontinuation
- 2005-06-28 MX MXPA06015032A patent/MXPA06015032A/es not_active Application Discontinuation
- 2005-06-28 AU AU2005260056A patent/AU2005260056B2/en not_active Ceased
- 2005-06-28 MX MXPA06015192A patent/MXPA06015192A/es active IP Right Grant
- 2005-06-28 PE PE2005000754A patent/PE20060524A1/es not_active Application Discontinuation
- 2005-06-28 JP JP2007519416A patent/JP2008504368A/ja not_active Withdrawn
- 2005-06-28 AU AU2005259894A patent/AU2005259894C1/en not_active Ceased
- 2005-06-28 KR KR1020067027370A patent/KR20070037448A/ko not_active Ceased
- 2005-06-28 KR KR1020067027376A patent/KR20070028458A/ko not_active Ceased
- 2005-06-28 JP JP2007519390A patent/JP4782117B2/ja not_active Expired - Fee Related
- 2005-06-28 JP JP2007519322A patent/JP4860609B2/ja not_active Expired - Fee Related
- 2005-06-28 EP EP05764291A patent/EP1768983A2/en not_active Withdrawn
- 2005-06-28 BR BRPI0512722-0A patent/BRPI0512722A/pt not_active Application Discontinuation
- 2005-06-28 WO PCT/US2005/022682 patent/WO2006004636A2/en not_active Ceased
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2006
- 2006-12-25 IL IL180325A patent/IL180325A0/en unknown
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2007
- 2007-01-24 NO NO20070453A patent/NO20070453L/no not_active Application Discontinuation
- 2007-01-26 NO NO20070514A patent/NO20070514L/no not_active Application Discontinuation
- 2007-01-26 NO NO20070506A patent/NO20070506L/no not_active Application Discontinuation
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